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Solid dispersion and solid preparation of ulipristal acetate

A technology of ulipristal acetate and solid dispersion, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, which can solve the problem of low dissolution, achieve the best dissolution rate, and improve Dissolution amount, the effect of ensuring drug efficacy

Active Publication Date: 2013-04-03
SHANDONG CHUANGXIN PHARMA RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the extremely low dissolution status of ulipristal acetate products in insoluble media in the prior art, it is an urgent problem to be solved to develop a new preparation of ulipristal acetate with high bioavailability and high dissolution

Method used

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  • Solid dispersion and solid preparation of ulipristal acetate
  • Solid dispersion and solid preparation of ulipristal acetate
  • Solid dispersion and solid preparation of ulipristal acetate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1 prepares the solid preparation of ulipristal acetate

[0022]

[0023] The preparation method is as follows: take 30 g of ulipristal acetate and 150 g of lactose, and mill them in a ball mill for 30 minutes to obtain a solid dispersion of ulipristal acetate; take 180 g of the solid dispersion, add 87 g of lactose, 15 g of povidone, and add appropriate amount of purified water Prepare into granules, add crospovidone and magnesium stearate after drying, mix well and press into tablets to obtain ulipristal acetate tablets.

[0024] The following examples are prepared for the solid dispersion of ulipristal acetate

Embodiment 2

[0026] Name of raw material Amount (g)

[0027] Ulipristal acetate 30

[0028] Lactose 90

[0029] The preparation method is as follows: take ulipristal acetate and lactose and ball mill for 45 minutes in a ball mill to obtain a solid dispersion of ulipristal acetate.

Embodiment 3

[0031] Name of raw material Amount (g)

[0032] Ulipristal acetate 30

[0033] Lactose 300

[0034] The preparation method is as follows: take ulipristal acetate and lactose and ball mill for 30 minutes in a ball mill to obtain the ulipristal acetate solid dispersion.

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Abstract

The invention discloses solid dispersion of ulipristal acetate which is prepared from 1 part by weight of ulipristal acetate and 3-20 parts by weight of auxiliary material, wherein the auxiliary material is one or combination of more than two selected from lactose, mannitol, sorbitol and povidone. The invention also discloses a solid preparation of the ulipristal acetate which is prepared from the solid dispersion of the ulipristal acetate and the conventional preparation auxiliary material, wherein the conventional preparation auxiliary material comprises filler, a disintegrating agent, a binding agent, a lubricating agent or flow aid. The solid preparation of the ulipristal acetate disclosed by the invention has higher dissolution rate compared with the ulipristal acetate tablet disclosed by the Chinese patent with the publication number of CN102245173A, the dissolution rate of the ullipristal acetate in a slightly soluble medium can be greatly increased, further bioavailability of the ulipristal acetate is improved and a pharmaceutical effect is guaranteed.

Description

technical field [0001] The invention relates to a solid dispersion solid preparation of ulipristal acetate and a preparation method thereof. Background technique [0002] Ulipristal acetate is a selective progesterone receptor modulator. It is the first drug approved for emergency contraception within 120 hours in the world. It is insoluble in water and slightly soluble in 0.1mol / L hydrochloric acid solution. Publication No. The Chinese patent application of CN102245173A discloses a kind of ulipristal acetate tablet, has only described the stripping of this product in the hydrochloric acid solution of 0.1mol / L, and this prescription is in other media (water, pH4.5, 6.8 buffer solution) ) is extremely low, which obviously reduces the bioavailability of the product, which in turn may cause the failure of emergency contraception. Based on the extremely low dissolution status of ulipristal acetate products in insoluble media in the prior art, it is an urgent problem to be solve...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K9/16A61K31/56A61K47/32A61K47/26A61K47/10A61P15/18
Inventor 邢来田齐玉威邵涛明杨冬霞段连帅孙振江秦玉荣娄艳华郝晓朋田兴华
Owner SHANDONG CHUANGXIN PHARMA RES & DEV
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